, Volume: 14( 2) DOI: 10.37532/ 2320-1967.2022. 14(2).161
Natural P-Glycoprotein Inhibitors as Chemopreventives
- Pankaj GuptaSchool of Medical and Allied Sciences, KR Mangalam University, Sohna Road, Gurgaon, Haryana, India., E-mail: [email protected]
Citation: Gupta P. Natural P-Glycoprotein Inhibitors as Chemopreventives. ChemXpress 2022;14(2):161.
P-glycoprotein (P-GP) is a transmembrane permeability glycoprotein belonging to the ATP binding cassette (ABC) super family that functions specifically as a carrier mediated primary active efflux transporter. P-GP was first discovered in 1976 for its role in multi-drug resistance in cancer.
Glycoprotein; Efflux transporter
P-glycoprotein (P-GP) is a transmembrane penetrability glycoprotein having a place with the ATP restricting tape (ABC) super family that capabilities explicitly as a transporter interceded essential dynamic efflux carrier. It is generally conveyed all through the body and has a different scope of substrates that incorporate a few imperative helpful specialists whose bioavailability is decreased or opposition is prompted in view of the protein efflux. P-GP was first found in 1976 for its job in multi-drug opposition in malignant growth; it is over communicated in a few human cancers and is a significant boundary to outcome in disease therapy. Because of its job in drug digestion, P-GP has extensive clinical significance as it influences the retention, appropriation and emission of anticancer medications. A few regular items from plants and marine sources have been accounted for their P-GP inhibitory activity and in this manner filling in as potential chemopreventives when co-directed with hostile to malignant growth specialists. The P-GP inhibitory mixtures from plant sources have a place with different classes like flavonoids, stilbenes, coumarins, terpenoids, alkaloids and saponins though the P-GP inhibitors from marine normal items have a place with the class of polyketides[1,2]. A few flavonoids have been accounted for to reveal P-GP hindrance, for example, flavonoids from grape natural product squeeze, for example, kaempferol and naringenin, flavonoid from Scutellariae radix viz. baicalein, procyanidine from bark of Pinus massoniana and so on. P-GP inhibitors from different classes incorporate resveratrol, a notable stilbene, and coumarins from foundations of Angelica gigas, dihydroxybergamotin and other furanocoumarins contained in grapefruit squeeze, for example, bergamotin, bergaptol and bergapten. Instances of alkaloids incorporate glaucine, cepharanthine and so on, illustration of diterpenes incorporate euphomelliferine, and instances of steroidal saponins incorporate primulanin, astragaloside II and karavelagenin C. Various P-GP inhibitors have been gotten from marine sources, for example, ecteinascidin 743 confined from Caribbean tunicate Ecteinascidia turbidata, discodermolide, a polyketides from wipe Discodermia dissoluta, bryostatin 1 from bryozoans Bugulia neritina and so on. These P-GP inhibitors from regular sources might go about as likely enhancers of bioavailability of different anticancer medications by forestalling the multi drug obstruction, decreasing the compelling portion of anticancer medications and their related secondary effects[3-5].
- 1.Nabekura T, Kamiyama S, Kitagawa S. Effects of dietary chemopreventive phytochemicals on P-glycoprotein function. Biochemical and biophysical research communications. 2005;327(3):866-70.
- 2. Engi H, Hohmann J, Gang G et. al. Chemoprevention and inhibition of P?glycoprotein in cancer cells by Chinese medicinal herbs..Phytotherapy Research: An International Journal Devoted to Pharmacological and Toxicological Evaluation of Natural Product Derivatives. 2008;22(12):1671-6.
- 3.Zhou S, Lim LY, Chowbay B. Herbal modulation of P?glycoprotein. Drug metabolism reviews. 2004;36(1):57-104.
- Dong J, Qin Z, Zhang WD et. al. Medicinal chemistry strategies to discover P-glycoprotein inhibitors: An update.. Drug Resistance Updates. 2020;49:100681.
- Jodoin J, Demeule M, Béliveau R. Inhibition of the multidrug resistance P-glycoprotein activity by green tea polyphenols..Biochimica et Biophysica Acta (BBA)-Molecular Cell Research. 2002;1542(13):149-59.